ANTIPROTOZOA MEDICINE

ARJO SURJANTO
SCHOOL OF NURSERY
BANDUNG POLYTECHNIC OF HEALTH
 MEDICATION OF MALARIA
There are 4 Plasmodium species cause malaria in human: P
vivax, P malariae, P ovale and P falciparum. Although they
could cause heavy malaria, P falciparum might cause the
most seriously complicated and death.
The effectively of malaria medicine variously depend
species and live stadium of parasite. On the other hand,
resisted parasite to the medicine might cause important
problem in medication.
P falciparum and P malariae would attack and multiplicity on
liver once only. Infection on liver spontaneous stopped in 4
weeks. Then, multiplication is going in erythrocyte. Hence,
eliminate this species need more than 4 weeks after
inoculation of sporozoit.
Meanwhile, P vivax (and perhaps P ovale) is inactivated
form (hypnozoit) and might be relapse caused infection.
Therefore, medication that eradication parasite from liver
and erythrocyte is important
 LIVE CYCLE OF MALARIA
PARASITE
HUMAN BODY
MOSQUITO BODY
Blood vessel
Male female Other
Paras
ite se erythrocyt
xual
fo rm
Sporozoit ERYTHROCYT
Gametocyt
ERYTHROCYTIC
STADIUM
Merozoit Merozoit
Sporozoit
Merozoit
HEPAR
Multiplication

EXOERYTHROCYTIC STADIUM
 CLASSIFICATION OF
ANTIPROTOZOA MEDICINE
Several main antiprotozoa agent is classified in chemical group (like
quinine, quinolin, quinacrine etc), other are antibiotics (tetracycline,
doxycycline), halofanthrine, and qinghaosu and its derivates. Regimen of
drugs is used to cure malaria included Fransidar (pyrimethamin
sulphadoxin) and Maloprim (pyrimethamin dapsone)
Malaria medicine might divided into its selectivity action of different live
phase of parasite. Medicines which eliminated tissue schizon growth or
latent hypnozid on liver are called tissue schizonticide. Medicine which
works against blood schizon is called as blood schizonticide or suppressive
agent (chloroquine, amodiaquine, proguanil, pyrimetamin, mefloquine,
quinine). Gametocide is medicine which prevent infection in mosquito body
by attacked gametocyte in blood (primaquine for P falciparum, and
chloroquine for P ovale, P vivax, and P malariae). When we would like to
prohibit gametocide infection to mosquito body, we could used
sporonticidal agent (pyrimethamin and proguanil)
There are not medicine that fully causal prophylactics except antiphol
(pyrimethamin and proguanil) that prevent initial maturity of hepatic schizon
P falsiparum. However, blood schizonticide could shatter plasmodium on
blood circulation (that prevent attack), when used in enough time, it could
curing P falsiparum and P malariae. Primaquin shatter hypnozoit of P vivax
and P ovale on liver and when used together with blood schizonticide,
radical effect could kill certain infection
 PROPHYLAXIS AND
MEDICATION
When client is recommended to use
prophylaxis medicine, he or she might
thing about preventing to mosquito bites
eradication of mosquito nest look like
better
There are several prophylactic medicines
as mefloquin, and primaquin
 CHLOROQUINE (1)
Chloroquine is used as chemo suppressant and medicine of malaria, except fully or
part resistance of P falsiparum strain. This medicine is used too medication of hepatic
amoebiasis. Hydroxychloroquine (a derivate of chloroquine) had characteristic almost
identical.
Phosphate salt of chloroquine is used orally, while hydrochloride is parentherally
It is rapid and almost fully absorption from digest tract. It reach maximum plasma
concentration (50 65% bind to protein) during 3 hours, and then rapid distribute to
body tissues. Since concentrated in tissue, distribution volume looked like so
voluminous (about 13,000 l) slow release and metabolite
Its distribution volume is great loading dose had to given when effective
concentration of plasma schizonticide needed on acute attack. This medicine is well
absorbed per i.m., but to prevent dangerous toxicity divided in several doses
Chloroqiune is effective blood schizonticide used to prevent or eradication attack of
malaria vivax, malaria ovale, sensitive malaria falsiparum, gametocide (of P vivax, P
ovale, and P malariae, but not for P falsiparum)
Chloroquine is inactive to preerythrocitic stadium plasmodium, and have not radical
effect to P vivax or P ovale because it do not eliminated liver stage parasite
The certain anti malaria mechanism of action is known yet. They guess that its
mechanism of action is based on selective toxicity.
Chloroquine easy pass away placenta barrier. Half time of chloroquine is going to 3
5 days, and excretion via urine. Kidney excretion increase by urine acidity
Chloroquine usually end fever in 24 48 hours, eradicate parasitemia in 48 72 hours
from acute attack of P vivax, P ovale, P malariae, and sensitive P falciparum.
Chloroquine is prefer prophylaxis to all types of malaria, except in resistance P
falciparum area.
Chloroquine is use together emetine as alternative medicine against liver abscess
caused amoeba
 MEFLOQUINE
Mefloquine is useful for prophylaxis and medication of resistance malaria falciparum (by
chloroquine and others). This medicine is effective as prophylaxis for P vivax, and might be
P ovale and P malariae
It recommended oral administered because of local irritation in parentheral intake.
Mefloquine is well absorption, and peak concentration of plasma achieve in 7 24 hours.
Single oral dose is 250 mg produces plasma concentration 290 340 ng/ml, advanced daily
dose would produce stable plasma concentration in 560 1250 ng/ml (chemosuppressive to
P falciparum achieved in plasma concentration 200 300 ng/ml). Mefloqiune is strong
bounding to plasma protein of erythrocyte, then extensively distributed to tissues included
CNS. Clearance is going on liver. It acid metabolite slowly excreted especially as faeces. Its
half time take place 13 33 hours, but could detected for several month after the end of
medication.
Mefloquine had strong activity to P falciparum and P vivax, but inactive to gametocyt P
falciparum or liver stadium of P vivax
Like quinidine, mefloquine had effect to heart
Mefloquine is an effective prophylaxis to chloroquine resistance P falciparum and curatively
when using every week for 4 weeks after leave endemic area
Mefloquine indicated to oral medication of P falciparum infection. Recommended dose is
single dose of 1250 mg
Side effect in prophylaxis dose is minor like digest tract disorder, dizziness, painful, syncope
and extrasystole. When therapeutical dose especially over than 100mg, it happens digest
tract disorder, weakness, and neuropsichiatric symptom much more than in prophylaxis
dose. Reaction could happen 2 3 weeks after medication stopped.
Contraindication of mefloquine is epilepsy or psychiatry disorder. This medicine also
prohibit to children with body weigh 15 kg or under 2 years. Contraindication also happen
when combine to quinine, quinidine, beta blocker, or Ca access inhibitor, or others
conducted heart. Administration of mefloquine just taken 12 hours after cosumption of
quinine or quinidine.
Prohibition should be taken to pregnant and fertile women, and individual which good
coordination and stereo difference needed. Also, patient administered anti convulsant
 AMOEBIASIS MEDICATION
Amoebiasis could appear heavy intestinal infection (dysentery), or light-medium symptom or
nonsymptomatic
Amoebiasis also could appear as amoeboma, liver abscess, or other extraintestinal infections.
All of antiamoeba agents work to Entamoeba hystolitica trophozoit, but inactive to cyste
stadium
Nitroimidazol (metronidazole, tynidazole, ornidazole) and emetin (and dehydroemetin) is
effective to eliminate organism intestinal, but ineffective for lumen
Chloroquine is used for liver amoebicide
In the case of luminal amoebicide, we could using dichloroacetamide (diclosanid furoate,
clefamid, teclozan, etofamid), halogenated hydroxyquinolone (Iodoquinol, clioquinol), and
antibiotics (oral tetracycline, paromomycine and erythromycine)
Clients with asymptomatic infection must be treated symptomatic infection or transmitted to
others. Drug of choice is diclosanid furoate and iodoquinol. Diclosanid prefer than iodoquinol
on side effects. Other alternative paromomycine or combination of metronidazole
iodoquinol/diclosanid
Light up to mild intestinal infection needed either luminal or tissues amoebicide. Parasites
should be eradicated from lumen, intestine wall, and liver. Combination of choice is
metronidazole diclosanid furoate or iodoquinol. Alternative combination is luminal amoebicide
tetracycline followed by chloroquine
Heavy intestinal infection therapy is similar to light mild infection. In this case, liquid
electrolyt and opioid are needed as control supporting of intestine motility
Hepatic abscess the client should be treated and rest. Medication of choice usually
metronidazol for 10 days. Luminal amoebicide (diclosanid furoate, iodoquinol or metronidazole)
would be added. Metronidazol is prefer because of its activity on anaerobic bacteria
Amoeboma (extraintestinal amoebiasis) drug of choice : metronidazole. Chloroquine is
alternative
 TRICHOMONIASIS AND GIARDIASIS
MEDICATION (1)
METRONIDAZOLE
Metronidazole is drug of choice to medication of urethra tract and as an
alternative drug to medication Giardia lamblia, Balantidium coli, Blastosistis
hominis, and intestinal and extraintestinal amoebiasis infection
Oral administration of metronidazol is rapid absorption and pass away all tissues
included cerebrospinalis liquid, breast milk and bone alveolar. Intracellular
concentration rapid achieves extracellular level. Half time of drug is 7.5 hours.
Medicine and its metabolite are excreted via urine. Clearance of plasma
metronidazol is decrease since liver disorder
Nitro group of metronidazol is derived by pheredoxine (or metabolic process
related pheredoxine). This chemical group is responsible to kill organism by react
to intracellular macromolecul. Hence, its derivate is responsible to medicine
bactericidal (not bacteriostatic) action to anaerobic bacteria
Metronidazole had a radio sensitization to tumor cell.
Metronidazole could killing trophozoit Entamoeba hystolitica but not its cyste
form
Dose of trichomoniasis urogenital : 3 X 250 mg per oral per day for 7 days. Single
dose of 2 g or 2 X 1 g effectively too. Sexual pair should be cured simultaneously.
Administration to pregnant women must be cancelled up to first trimester.
Dose of B giardiasis per oral is 3 X 250 mg a day for several days. Pediatric: 3 X 5
mg/kg BW/day for 5 days
Dose of balantidiasis: when tetracycline is ineffective, metronidazole is given 3 X
750 mg/day for 5 days
 TRICHOMONIASIS AND GIARDIASIS
MEDICATION (2)
Dose of Gardnerella vaginalis: oral administration is 2 X 500 mg/day for 5
days only for refracter infection
Dose of anaerobic infection: 2 X 500 mg daily for 5 days metronidazole is
used for post operation of appendectomy, colorectal surgery, and
abdominal hysterectomy
Dose of Fagedenic ulcus on foot, acute ulcerative ginggivitis, oris
cancrum, decubitus ulcus, lession caused other indolen: 3 X 250 mg
metronidazole daily by suitable medicine for anaerobic infection and
topical application are increasing curing and releasing of sickness,
edema inflamed, and purulent liquid.
Side effects are expressed as nausea, dry mouth, or metallic taste in
tongue sometimes happen. Darkness or brownish red of urine might be
happen. Others: vomiting, diarrhea, insomnia, weakness, dizziness,
stomatitis, rash, burn sensation in urethra, vertigo and paresthesia.
Metronidazole had effect resemble disulfiram, hence nausea and
vomiting might happen when alcohol consume together (24 hours before
and 48 hours after)
Caution should be taken on polypharmacy, long prescription especially
on client with hematology disorder historical
Metronidazole prefers prohibition on pregnancy (especially first
trimester) and lactation, and teenagers